US6333419B1 - Chromatographic separation method of paclitaxel and cephalomannin - Google Patents

Chromatographic separation method of paclitaxel and cephalomannin Download PDF

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Publication number
US6333419B1
US6333419B1 US09/724,504 US72450400A US6333419B1 US 6333419 B1 US6333419 B1 US 6333419B1 US 72450400 A US72450400 A US 72450400A US 6333419 B1 US6333419 B1 US 6333419B1
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United States
Prior art keywords
paclitaxel
cephalomannin
starting material
butyl
solvent
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Expired - Lifetime
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US09/724,504
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English (en)
Inventor
Bruno Gabetta
Gianfranco Zini
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Indena SpA
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Indena SpA
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Priority to US09/724,504 priority Critical patent/US6333419B1/en
Assigned to INDENA S.P.A. reassignment INDENA S.P.A. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: GABETTA, BRUNO, GIANFRANCO, ZINI
Priority to HU0204028A priority patent/HU229096B1/hu
Priority to AT01998544T priority patent/ATE427305T1/de
Priority to HK03102398.1A priority patent/HK1050523B/xx
Priority to DK01998544T priority patent/DK1392669T3/da
Priority to KR1020027009572A priority patent/KR100842457B1/ko
Priority to CZ20022490A priority patent/CZ304180B6/cs
Priority to JP2002546532A priority patent/JP4177665B2/ja
Priority to PL355683A priority patent/PL202590B1/pl
Priority to CNB018041345A priority patent/CN1187347C/zh
Priority to RU2002120482/04A priority patent/RU2276669C2/ru
Priority to ES01998544T priority patent/ES2321160T3/es
Priority to DE60138229T priority patent/DE60138229D1/de
Priority to PCT/EP2001/012982 priority patent/WO2002044162A1/en
Priority to CA002398405A priority patent/CA2398405C/en
Priority to PT01998544T priority patent/PT1392669E/pt
Priority to SK1092-2002A priority patent/SK287109B6/sk
Priority to IL15090101A priority patent/IL150901A0/xx
Priority to SI200130911T priority patent/SI1392669T1/sl
Priority to AU19085/02A priority patent/AU780761B2/en
Priority to EP01998544A priority patent/EP1392669B1/en
Priority to ARP010105483A priority patent/AR031511A1/es
Publication of US6333419B1 publication Critical patent/US6333419B1/en
Application granted granted Critical
Priority to IL150901A priority patent/IL150901A/en
Priority to NO20023555A priority patent/NO328356B1/no
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D305/00Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/14Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01DSEPARATION
    • B01D15/00Separating processes involving the treatment of liquids with solid sorbents; Apparatus therefor
    • B01D15/08Selective adsorption, e.g. chromatography
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N5/00Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
    • C12N5/04Plant cells or tissues

Definitions

  • a mixture containing 70 g paclitaxel and 30 g cephalomannin is dissolved in 1.5 L t-butyl formate and loaded onto a column containing 10 kg silica gel suspended in the same solvent.
  • the column is eluted with t-butyl formate, and the fractions are joined after HPLC/TLC analysis.
  • the fractions containing paclitaxel and cephalomannin are concentrated to dryness separately and the residues crystallized by acetone and heptane in suitable rations to yield paclitaxel and cephalomannin having a HPLC purity over 99%.

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Botany (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Cell Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Microbiology (AREA)
  • Analytical Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Epoxy Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines Containing Plant Substances (AREA)
US09/724,504 2000-11-28 2000-11-28 Chromatographic separation method of paclitaxel and cephalomannin Expired - Lifetime US6333419B1 (en)

Priority Applications (24)

Application Number Priority Date Filing Date Title
US09/724,504 US6333419B1 (en) 2000-11-28 2000-11-28 Chromatographic separation method of paclitaxel and cephalomannin
DE60138229T DE60138229D1 (de) 2000-11-28 2001-11-09 Verfahren zur chromatographischen trennung von paclitaxel und cephalomannin
CA002398405A CA2398405C (en) 2000-11-28 2001-11-09 Chromatographic separation method of paclitaxel and cephalomannin
HK03102398.1A HK1050523B (en) 2000-11-28 2001-11-09 Chromatographic separation method of paclitaxel and cephalomannin
DK01998544T DK1392669T3 (da) 2000-11-28 2001-11-09 Fremgangsmåde til chromatografisk adskillelse af paclitaxel og cephalomannin
KR1020027009572A KR100842457B1 (ko) 2000-11-28 2001-11-09 파클리탁셀 및 세팔로만닌의 크로마토그래피에 의한분리방법
CZ20022490A CZ304180B6 (cs) 2000-11-28 2001-11-09 Chromatografická metoda separace paclitaxelu a cefalomaninu
JP2002546532A JP4177665B2 (ja) 2000-11-28 2001-11-09 パクリタクセルとセフアロマンニンのクロマトグラフ分離法
PL355683A PL202590B1 (pl) 2000-11-28 2001-11-09 Sposób chromatograficznego rozdzielania paclitaxelu i cefalomanniny
CNB018041345A CN1187347C (zh) 2000-11-28 2001-11-09 紫杉醇和三尖杉宁碱的层析分离方法
RU2002120482/04A RU2276669C2 (ru) 2000-11-28 2001-11-09 Способ хроматографического разделения паклитаксела и цефаломаннина
ES01998544T ES2321160T3 (es) 2000-11-28 2001-11-09 Metodo de separacion cromatigrafica de paclitaxel y cefalomanina.
HU0204028A HU229096B1 (hu) 2000-11-28 2001-11-09 Eljárás paclitaxel és cefalomannin kromatográfiás elválasztására
PCT/EP2001/012982 WO2002044162A1 (en) 2000-11-28 2001-11-09 Chromatographic separation method of paclitaxel and cephalomannin
AT01998544T ATE427305T1 (de) 2000-11-28 2001-11-09 Verfahren zur chromatographischen trennung von paclitaxel und cephalomannin
PT01998544T PT1392669E (pt) 2000-11-28 2001-11-09 Método de separação cromatográfica de paclitaxel e cefalomanina
SK1092-2002A SK287109B6 (sk) 2000-11-28 2001-11-09 Spôsob separácie paclitaxelu od cefalomanínu
IL15090101A IL150901A0 (en) 2000-11-28 2001-11-09 Chromatographic separation method of paclitaxel and cephalomannin
SI200130911T SI1392669T1 (sl) 2000-11-28 2001-11-09 Postopek za kromatografsko separacijo paklitaksela in cefalomanina
AU19085/02A AU780761B2 (en) 2000-11-28 2001-11-09 Chromatographic separation method of paclitaxel and cephalomannin
EP01998544A EP1392669B1 (en) 2000-11-28 2001-11-09 Chromatographic separation method of paclitaxel and cephalomannin
ARP010105483A AR031511A1 (es) 2000-11-28 2001-11-26 Metodo de separacion cromatografica de paclitaxel y cefalomanina
IL150901A IL150901A (en) 2000-11-28 2002-07-25 Chromatographic separation of paclitaxel and splumanin
NO20023555A NO328356B1 (no) 2000-11-28 2002-07-25 Kromatografisk separasjonsmetode av paclitaxel og cefalomannin

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US09/724,504 US6333419B1 (en) 2000-11-28 2000-11-28 Chromatographic separation method of paclitaxel and cephalomannin

Publications (1)

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US6333419B1 true US6333419B1 (en) 2001-12-25

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US09/724,504 Expired - Lifetime US6333419B1 (en) 2000-11-28 2000-11-28 Chromatographic separation method of paclitaxel and cephalomannin

Country Status (22)

Country Link
US (1) US6333419B1 (cs)
EP (1) EP1392669B1 (cs)
JP (1) JP4177665B2 (cs)
KR (1) KR100842457B1 (cs)
CN (1) CN1187347C (cs)
AR (1) AR031511A1 (cs)
AT (1) ATE427305T1 (cs)
AU (1) AU780761B2 (cs)
CA (1) CA2398405C (cs)
CZ (1) CZ304180B6 (cs)
DE (1) DE60138229D1 (cs)
DK (1) DK1392669T3 (cs)
ES (1) ES2321160T3 (cs)
HU (1) HU229096B1 (cs)
IL (2) IL150901A0 (cs)
NO (1) NO328356B1 (cs)
PL (1) PL202590B1 (cs)
PT (1) PT1392669E (cs)
RU (1) RU2276669C2 (cs)
SI (1) SI1392669T1 (cs)
SK (1) SK287109B6 (cs)
WO (1) WO2002044162A1 (cs)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060014968A1 (en) * 2004-07-15 2006-01-19 Indena S.P.A. Methods for obtaining paclitaxel from taxus plants
WO2006014356A1 (en) * 2004-07-02 2006-02-09 Ivax Pharmaceuticals S.R.O. Process for the isolation of paclitaxel
WO2006014345A1 (en) * 2004-07-02 2006-02-09 Ivax Pharmaceuticals S.R.O. Process for the separation of paclitaxel and cephalomannin
CN104251896A (zh) * 2014-09-30 2014-12-31 江苏红豆杉药业有限公司 一种半合成紫杉醇的质量控制方法
CN104262300A (zh) * 2014-09-30 2015-01-07 江苏红豆杉药业有限公司 一种除去紫杉醇中三尖杉宁碱的方法

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE602004008903T2 (de) * 2004-07-13 2008-06-19 Indena S.P.A. Verfahren zur Gewinnung von Paclitaxel aus Taxuspflanzen
CN102219764B (zh) * 2011-05-12 2013-06-26 河南省科学院化学研究所有限公司 一种工业化分离纯化紫杉醇的方法
KR102263764B1 (ko) * 2014-08-13 2021-06-09 주식회사 엘지생활건강 세팔로만닌 또는 이의 약학적으로 허용가능한 염을 포함하는 피부 미백 또는 항염증용 화장료 또는 약학 조성물
CN113512015A (zh) * 2021-05-26 2021-10-19 上海卓鼎生物技术有限公司 一种工业化提纯三尖杉宁碱的方法

Citations (4)

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US5618538A (en) 1991-04-19 1997-04-08 The University Of Mississippi Methods and compositions for isolating taxanes
US5670673A (en) 1990-11-02 1997-09-23 University Of Florida Method for the isolation and purification of taxol and its natural analogues
US5856532A (en) 1996-08-14 1999-01-05 Council Of Scientific & Industrial Research Process for the production of taxol
US6002025A (en) 1999-02-24 1999-12-14 Bcm Developement Inc. Method for the purification of taxanes

Family Cites Families (4)

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FR2703049B1 (fr) * 1993-03-22 1995-04-21 Rhone Poulenc Rorer Sa Procédé de purification des taxoïdes.
WO1997009443A1 (en) 1995-09-05 1997-03-13 Michigan State University PROCESS FOR THE ISOLATION AND PURIFICATION OF TAXOL AND TAXANES FROM TAXUS spp
US6136989A (en) * 1998-12-30 2000-10-24 Phytogen Life Sciences, Incorporated Method for high yield and large scale extraction of paclitaxel from paclitaxel-containing material
US5969165A (en) * 1999-01-07 1999-10-19 508037 (Nb) Inc. Isolation and purification of paclitaxel and other related taxanes by industrial preparative low pressure chromatography on a polymeric resin column

Patent Citations (4)

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US5670673A (en) 1990-11-02 1997-09-23 University Of Florida Method for the isolation and purification of taxol and its natural analogues
US5618538A (en) 1991-04-19 1997-04-08 The University Of Mississippi Methods and compositions for isolating taxanes
US5856532A (en) 1996-08-14 1999-01-05 Council Of Scientific & Industrial Research Process for the production of taxol
US6002025A (en) 1999-02-24 1999-12-14 Bcm Developement Inc. Method for the purification of taxanes

Non-Patent Citations (14)

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Beckvermit et al., "An improved method for separating paclitaxel and cephalomannine using ozone and girard reagents", J. Org. Chem., 61, 9038-9040, 1996.
Blechert et al., "Mise en evidence de nouveaux analogues du taxol extraits de taxus baccata", Journal of Natural Products, vol. 47, No. 1, 131-137, 1984.
Chmurny et al., "H- and C-NMR assignment for taxol, 7-epi-taxol, and cephalomannine", Journal of Natural Products, vol. 55, 414-423, 1992.
Falzone et al., "Characterization of taxol in methylene chloride by NMR spectroscopy", 33(9), pp. 1169-1172, 1992.
J.H. Cardellina, "HPLC Separation of Taxol and Cephalomannine", Journal of Liquid Chromatography, 14,659-665, 1991.
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Kingston et al., "Modified taxols, 7. A method for the separation of taxol and cephalomannine", Journal of Natural Products, vol. 55, No. 2, 259-261, 1992.
M.C. Wani et al., "Plant Antitumor Agents VI. The Isolation and Structure of Taxol, A Novel Antileukemic and Antitumor Agent From Taxus Brevifolia," J. Amer. Chem. Soc., 93, (9), 2325-2327, 1971.
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Witherup et al., High performance liquid chromatographic separation of taxol and related compounds from taxus brevifolia:, Journal of Liquid Chromatography, 12(11), 2117-2132, 1989.

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006014356A1 (en) * 2004-07-02 2006-02-09 Ivax Pharmaceuticals S.R.O. Process for the isolation of paclitaxel
WO2006014345A1 (en) * 2004-07-02 2006-02-09 Ivax Pharmaceuticals S.R.O. Process for the separation of paclitaxel and cephalomannin
US20080214847A1 (en) * 2004-07-02 2008-09-04 Ivax Pharmaceuticals S.R.O. Process for the Separation of Paclitaxel and Cephalomannin
US20060014968A1 (en) * 2004-07-15 2006-01-19 Indena S.P.A. Methods for obtaining paclitaxel from taxus plants
US7112687B2 (en) * 2004-07-15 2006-09-26 Indena, S.P.A. Methods for obtaining paclitaxel from taxus plants
CN104251896A (zh) * 2014-09-30 2014-12-31 江苏红豆杉药业有限公司 一种半合成紫杉醇的质量控制方法
CN104262300A (zh) * 2014-09-30 2015-01-07 江苏红豆杉药业有限公司 一种除去紫杉醇中三尖杉宁碱的方法
CN104251896B (zh) * 2014-09-30 2016-07-20 江苏红豆杉药业有限公司 一种半合成紫杉醇的检测方法

Also Published As

Publication number Publication date
KR100842457B1 (ko) 2008-07-01
HK1050523A1 (en) 2003-06-27
CA2398405A1 (en) 2002-06-06
KR20020068088A (ko) 2002-08-24
CA2398405C (en) 2010-01-12
CZ304180B6 (cs) 2013-12-11
DK1392669T3 (da) 2009-05-18
RU2276669C2 (ru) 2006-05-20
SK10922002A3 (sk) 2003-01-09
IL150901A0 (en) 2003-02-12
JP4177665B2 (ja) 2008-11-05
HU229096B1 (hu) 2013-07-29
SI1392669T1 (sl) 2009-06-30
AR031511A1 (es) 2003-09-24
HUP0204028A3 (en) 2004-01-28
NO328356B1 (no) 2010-02-01
PT1392669E (pt) 2009-04-20
NO20023555D0 (no) 2002-07-25
EP1392669B1 (en) 2009-04-01
WO2002044162A1 (en) 2002-06-06
ATE427305T1 (de) 2009-04-15
PL355683A1 (en) 2004-05-17
CN1396917A (zh) 2003-02-12
CZ20022490A3 (cs) 2002-10-16
HUP0204028A2 (en) 2003-05-28
AU780761B2 (en) 2005-04-14
JP2004514715A (ja) 2004-05-20
PL202590B1 (pl) 2009-07-31
AU1908502A (en) 2002-06-11
ES2321160T3 (es) 2009-06-03
NO20023555L (no) 2002-09-30
IL150901A (en) 2010-11-30
DE60138229D1 (de) 2009-05-14
CN1187347C (zh) 2005-02-02
SK287109B6 (sk) 2009-12-07
RU2002120482A (ru) 2004-01-10
EP1392669A1 (en) 2004-03-03

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